Biochemometry-Based Discovery of Phenylpropanoids from Azadirachta indica Fruits as Inhibitors of In Vitro Osteoclast Formation

Ammar Tahir, Carina Kampleitner, Theresa Wirglauer, Ulrike Grienke, Oskar Hoffmann, Judith M. Rollinger

Publications: Contribution to journalArticlePeer Reviewed

Abstract

(1) Background: Inhibition of osteoclast differentiation is the key approach in treating osteoporosis. However, using state-of-the-art treatments such as bisphosphonates and estrogen-based therapy is usually accompanied by many side effects. As opposed to this, the use of natural products as an osteoporotic remedy delivers promising outcomes with minimal side effects. (2) Methods: In the present study, we implemented a biochemometric workflow comprising (i) chemometric approaches using NMR and mass spectrometry and (ii) cell biological approaches using an osteoclast cytochemical marker (TRAP). The workflow serves as a screening tool to pursue potential in vitro osteoclast inhibitors. (3) Results: The workflow allowed for the selective isolation of two phenylpropanoids (coniferyl alcohol and sinapyl alcohol) from the fruits of neem tree (Azadirachta indica). These two isolated phenylpropanoids showed a very promising dose-dependent inhibition of osteoclast differentiation with negligible effects in terms of cell viability. (4) Conclusion: The presented workflow is an effective tool in the discovery of potential candidates for osteoclast inhibition from complex extracts. The used biochemometric approach saves time, effort and costs while delivering precise hints to selectively isolate bioactive constituents.

Original languageEnglish
Article number3611
Number of pages13
JournalMolecules
Volume27
Issue number11
DOIs
Publication statusPublished - 4 Jun 2022

Austrian Fields of Science 2012

  • 104013 Natural product chemistry

Keywords

  • ACTIVATION
  • Azadirachta indica
  • CONSTITUENTS
  • DIFFERENTIATION
  • ESTROGEN
  • MECHANISMS
  • NF-KAPPA-B
  • PRECURSORS
  • biochemometry
  • inhibition of osteoclast differentiation
  • osteoporosis
  • phenylpropanoids
  • Fruit
  • Azadirachta/chemistry
  • Osteoclasts
  • Plant Extracts/pharmacology

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